Assay Detail
Binding
CHEMBL673590
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Tissue |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.48 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303313 | — | — | 1 | 9.40 |
| CHEMBL426763 | — | — | 1 | 9.37 |
| CHEMBL369367 | — | — | 1 | 9.35 |
| CHEMBL7617 | — | — | 1 | 9.00 |
| CHEMBL177455 | — | — | 1 | 8.46 |
| CHEMBL64875 | — | — | 1 | 8.44 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.32 |
| CHEMBL366679 | — | — | 1 | 8.07 |
| CHEMBL367045 | — | — | 2 | 7.77 |
| CHEMBL831 | LOXAPINE | 4.0 | 1 | 7.68 |
| CHEMBL415300 | ISOCLOZAPINE | — | 1 | 7.33 |
| CHEMBL368324 | — | — | 1 | 7.30 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 7.16 |
| CHEMBL176169 | — | — | 1 | 6.90 |
| CHEMBL367087 | — | — | 1 | 6.90 |
| CHEMBL7828 | ISOLOXAPINE | — | 1 | 6.82 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.60 |
| CHEMBL275696 | — | — | 1 | 6.28 |
| CHEMBL367180 | — | — | 1 | 6.07 |
| CHEMBL362060 | — | — | 1 | 5.87 |
| CHEMBL175226 | — | — | 1 | 5.84 |
| CHEMBL367875 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303313 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL426763 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL369367 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL7617 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL177455 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL64875 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL366679 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL367045 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL367045 | — | Ki | = | 17.2 | nM | 7.76 |
| CHEMBL831 | LOXAPINE | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL415300 | ISOCLOZAPINE | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL368324 | — | Ki | = | 49.6 | nM | 7.30 |
| CHEMBL715 | OLANZAPINE | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL367087 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL176169 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL7828 | ISOLOXAPINE | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL42 | CLOZAPINE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL275696 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL367180 | — | Ki | = | 854.0 | nM | 6.07 |
| CHEMBL362060 | — | Ki | = | 1345.0 | nM | 5.87 |
| CHEMBL175226 | — | Ki | = | 1430.0 | nM | 5.84 |
| CHEMBL367875 | — | Ki | = | 3824.0 | nM | 5.42 |